DEFINITION
GLP-1 receptor agonists (GLP-1 RAs) are compounds — mostly peptides — that bind and activate the glucagon-like peptide-1 receptor (GLP-1R), reproducing the physiological actions of native GLP-1 with markedly extended pharmacokinetics.
Modern long-acting GLP-1 RAs such as Semaglutide combine DPP-4 resistance with albumin-binding acylation to achieve plasma half-lives measured in days rather than minutes. Dual (Tirzepatide) and triple (Retatrutide) agonists extend the design principle to additional incretin-family receptors.
WHY IT MATTERS
The GLP-1 RA class is the central reference class against which every dual and triple incretin agonist is benchmarked.
RELATED
Compounds